For research use only. Not for therapeutic Use.
WDR5-0103 is a potent and selective WD repeat-containing protein 5 (WDR5) antagonist with Kd of 450 nM.
IC50 value: 450 nM (Kd)
Target: WDR5
in vitro: WDR5-0103 inhibits MLL catalytic activity with an IC50 value of 39±10 μM. An increase in MLL complex concentration resulted in proportional increase in IC50 values for WDR5-0103 (83±10 and 280±12 μM at concentrations of 500 and 1000 nM of the core trimeric MLL complex respectively). These data are consistent with a mechanism of action in which WDR5-0103 antagonizes the interaction of WDR5 with MLL by competing with MLL for their mutual binding site on WDR5.
| Catalog Number | I013783 |
| CAS Number | 890190-22-4 |
| Synonyms | methyl 3-[(3-methoxybenzoyl)amino]-4-(4-methylpiperazin-1-yl)benzoate |
| Molecular Formula | C21H25N3O4 |
| Purity | ≥95% |
| InChI | InChI=1S/C21H25N3O4/c1-23-9-11-24(12-10-23)19-8-7-16(21(26)28-3)14-18(19)22-20(25)15-5-4-6-17(13-15)27-2/h4-8,13-14H,9-12H2,1-3H3,(H,22,25) |
| InChIKey | ZPLBXOVTSNRBFB-UHFFFAOYSA-N |
| SMILES | CN1CCN(CC1)C2=C(C=C(C=C2)C(=O)OC)NC(=O)C3=CC(=CC=C3)OC |
| Reference | [1]. Senisterra G, et al. Small-molecule inhibition of MLL activity by disruption of its interaction with WDR5. Biochem J. 2013 Jan 1;449(1):151-159. |
